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TargetTransient receptor potential cation channel subfamily V member 1
LigandBDBM50056358
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1451403
IC50 3.0±n/a nM
Citation Voight, EAGomtsyan, ARDaanen, JFPerner, RJSchmidt, RGBayburt, EKDiDomenico, SMcDonald, HAPuttfarcken, PSChen, JNeelands, TRBianchi, BRHan, PReilly, RMFranklin, PHSegreti, JANelson, RASu, ZKing, AJPolakowski, JSBaker, SJGauvin, DMLewis, LRMikusa, JPJoshi, SKFaltynek, CRKym, PRKort, ME Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy. J Med Chem57:7412-24 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Transient receptor potential cation channel subfamily V member 1
Name:Transient receptor potential cation channel subfamily V member 1
Synonyms:Capsaicin receptor | OTRPC1 | Osm-9-like TRP channel 1 | Transient receptor potential cation channel subfamily V member 1 (TRPV1) | Transient receptor potential cation channel subfamily V member 1 (VR1/TRPV1) | Transient receptor potential cation channel subfamily V member 1(TRPV1) | TrpV1 | Vanilloid VR1 | Vanilloid receptor | Vanilloid receptor 1 | Vanilloid receptor 1 (TrpV1/Vr1) | Vanilloid receptor 1 (VRI/TRPV1)
Type:Protein
Mol. Mass.:94960.75
Organism:Homo sapiens (Human)
Description:Q8NER1
Residue:839
Sequence:
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP
VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE
AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI
ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT
KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA
DNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE
PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN
RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL
SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS
MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE
DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF
IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA
FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS
SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50056358
NameBDBM50056358
Synonyms:CHEMBL3326581
TypeSmall organic molecule
Emp. Form.C22H22FN3O2
Mol. Mass.379.4274
SMILESCc1cc2c(NC(=O)N[C@@H]3CC(C)(C)Oc4cc(F)ccc34)cccc2cn1 |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a